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Compound Detail

CHEMBL491348

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CC(=O)c1c(Nc2ccc(Cl)cc2Cl)[nH]c2c([N+](=O)[O-])cc(Cl)cc2c1=O

Basic Information

ChEMBL ID CHEMBL491348
Phase Preclinical
Structure Type MOL
InChI Key RPOGXQPJVKMLKU-UHFFFAOYSA-N
5
Targets
6
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

426.6
MW (Da)
5.34
ALogP
5
HBA
2
HBD
105.1
PSA (Ų)
0.33
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H10Cl3N3O4
MW 426.64
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.10

Activity Summary

IC50 6 meas. best 7.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin D
CHEMBL2581
IC50 7.38 7.38 42.0 1
Calpain-1 catalytic subunit
CHEMBL3891
IC50 5.5 5.415 3160.0 2
Cathepsin B
CHEMBL4072
IC50 4.9 4.9 12690.0 1
Procathepsin L
CHEMBL3837
IC50 4.7 4.7 19820.0 1
Pro-cathepsin H
CHEMBL2225
IC50 4.49 4.49 32570.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19419206 10.1021/jm8014734 Calpain-1 catalytic subunit 2
19419206 10.1021/jm8014734 Cathepsin B 1
19419206 10.1021/jm8014734 Procathepsin L 1
19419206 10.1021/jm8014734 Pro-cathepsin H 1
19419206 10.1021/jm8014734 Cathepsin D 1

Data from ChEMBL 36 via Core Engine